Assay Detail
Binding
CHEMBL5735701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition In Vito Assay: The investigations on the inhibition of the recombinant TASK-1 and TASK-3 channels were carried out using stably transfected CHO cells. Here, the compounds according to the invention were tested with administration of 40 mM of potassium chloride in the presence of a voltage-sensitive dye for high-throughput screening of potassium channel from Molecular Devices FLIPR Application Note: Measuring membrane potential using the FLIPR membrane potential assay kit on Fluorometric Imaging Plate Reader (FLIPR) systems. The activity of the test substances was determined as their ability to inhibit a depolarization induced in the recombinant cells by 40 mM potassium chloride.
258
Total Activities
77
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Potassium channel subfamily K member 9 (CHEMBL2321614) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-phenyl-3-(piperazinomethyl)imidazo[1,2-A]pyridine derivatives as blockers of task-1 and task-2 channels, for the treatment of sleep-related breathing disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 86 | 6.76 | 8.98 |
| kon | 86 | - | - |
| k_off | 86 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6016320 | — | — | 6 | 8.98 |
| CHEMBL5979320 | — | — | 6 | 8.64 |
| CHEMBL5948731 | — | — | 3 | 8.52 |
| CHEMBL6050684 | — | — | 3 | 8.28 |
| CHEMBL5781241 | — | — | 6 | 8.21 |
| CHEMBL5928540 | — | — | 3 | 8.04 |
| CHEMBL5172358 | — | — | 3 | 8.03 |
| CHEMBL5932576 | — | — | 3 | 8.00 |
| CHEMBL5955132 | — | — | 3 | 7.96 |
| CHEMBL5936147 | — | — | 3 | 7.89 |
| CHEMBL5881187 | — | — | 3 | 7.85 |
| CHEMBL5189300 | — | — | 6 | 7.82 |
| CHEMBL5955974 | — | — | 3 | 7.80 |
| CHEMBL5922163 | — | — | 3 | 7.77 |
| CHEMBL5833962 | — | — | 3 | 7.77 |
| CHEMBL5883778 | — | — | 6 | 7.70 |
| CHEMBL5976530 | — | — | 6 | 7.55 |
| CHEMBL6056886 | — | — | 3 | 7.52 |
| CHEMBL5953514 | — | — | 6 | 7.42 |
| CHEMBL5877257 | — | — | 3 | 7.28 |
| CHEMBL5756587 | — | — | 3 | 7.22 |
| CHEMBL5918386 | — | — | 3 | 7.20 |
| CHEMBL5969271 | — | — | 3 | 7.20 |
| CHEMBL6028256 | — | — | 3 | 7.15 |
| CHEMBL5932536 | — | — | 6 | 7.10 |
| CHEMBL5742220 | — | — | 3 | 7.01 |
| CHEMBL5941398 | — | — | 3 | 7.00 |
| CHEMBL5870683 | — | — | 3 | 6.96 |
| CHEMBL6013481 | — | — | 3 | 6.92 |
| CHEMBL6058665 | — | — | 3 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6016320 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL5979320 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5948731 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6050684 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5781241 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5928540 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5172358 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5932576 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5955132 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5936147 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5881187 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5189300 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5955974 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6016320 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5922163 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5833962 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5979320 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5883778 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5883778 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL5976530 | — | IC50 | = | 27.9 | nM | 7.55 |
| CHEMBL5976530 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL6056886 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5953514 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL5189300 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5877257 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5781241 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5756587 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5918386 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5969271 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL6028256 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5932536 | — | IC50 | = | 79.6 | nM | 7.10 |
| CHEMBL5742220 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5941398 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5870683 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6058665 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL6013481 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5995367 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5822460 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5932536 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5885901 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5763659 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5767153 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5855154 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5937118 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5953514 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5870080 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL6061336 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL6049147 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL6001517 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL6003079 | — | IC50 | = | 350.0 | nM | 6.46 |